CN1839903A - Pharmaceutical composition containing glabrous sarcandra herb extract and its uses - Google Patents
Pharmaceutical composition containing glabrous sarcandra herb extract and its uses Download PDFInfo
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Abstract
The invention discloses a medicinal composition containing active ingredients extracted from glabrous sarcandra herb, including flavones, and/or saponin, and/or polysaccharides, or one or more of the following flavone active ingredients: isofraxidin-7-O-glucopyranoside, 5,7-dihydroxyl flavanone, 2',6'-dihydroxy-4'-methoxyl chalcone, pinostrobin, dihydromyricetin, Astilbin, naringenin 4',7-dimethyl ether.
Description
Technical field
The present invention relates to the plant amedica Herba Sarcandrae, specifically a kind of medical composition and its use that contains Herba Sarcandrae and equal genus plants extract.
Background technology
Herba Sarcandrae (Sarcandra glabra (Thunb) Nakai) is a Chloranthaceae Herba Pileae Scriptae platymiscium, and dry herb has another name called Herba Pileae Scriptae, Herba Pileae Scriptae, Ramulus Sambuci Williamsii, refutes bone tea, atrophic debility of bones wind etc.Be the perennial evergreen draft, be distributed in provinces such as Jiangxi, Anhui, Zhejiang, Hunan, Hubei, Sichuan, Guangdong, Guangxi, Jiangxi Province is the main place of production.Herba Sarcandrae has effects such as blood circulation promoting and blood stasis dispelling, pain relieving, heat-clearing and toxic substances removing.Be used for the treatment of common inflammation, rheumatic arthritis.Be used for assistant treating cancer modern age, multiple malignant tumor such as gastric cancer, cancer of pancreas, hepatocarcinoma, esophageal carcinoma, rectal cancer etc. were had auxiliary curative effect.ZHONGJIEFENG ZHUSHEYE, oral liquid, tablet are used for thrombocytopenic purpura patient increased platelets counts, also are used for assistant treating cancer.There is report Herba Sarcandrae total flavones class extract to can be used for platelet purpura and assistant treating cancer, but effective site does not reach the purity of (50% to 99%) more than 50%, effective ingredient purity does not reach the purity of (85% to 99%) more than 85%, does not more have the preparation of flavone effective part, effective part of saponin, polysaccharide effective site.Present commercially available ZHONGJIEFENG ZHUSHEYE, oral liquid, tablet are crude preparation by using.
Summary of the invention
The objective of the invention is to provide a kind of new medical composition and its use that contains Herba Sarcandrae extract, it contains flavone effective part, the effective ingredient that Herba Sarcandrae extracts, effective part of saponin, polysaccharide effective site.Its effective site reaches the purity of (50% to 99%) more than 50%, and effective ingredient purity reaches the purity of (85% to 99%) more than 85%.
Purpose of the present invention can take following method to realize:
A kind of pharmaceutical composition that contains Herba Sarcandrae extract, it is characterized in that it contains effective site and/or the effective ingredient that extracts from Herba Sarcandrae, comprise flavone, and/or saponin, and/or the effective site of polysaccharide, or in the following flavone effective ingredient one or several: isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether, the purity of the effective site that extracts in the described Herba Sarcandrae is 50% to 99%, and the purity of the effective ingredient that extracts in the described Herba Sarcandrae is 85% to 99%.
The form of described compositions comprises: tablet: comprise general oral, buccal tablet, chewable tablet, injection: comprise small-volume injection, big injection, injectable powder, Emulsion, suspension, pill, drop pill, capsule and soft capsule, granule, effervescent, oral liquid, syrup, Emulsion, mixture, slow releasing agent, controlled release agent, targeting preparation and other various preparations.
The described preparation of drug combination method that contains Herba Sarcandrae extract is characterized in that may further comprise the steps:
The extraction separation of total flavone part and composition:
The flavonoid total extract can select following a kind of method extraction to obtain:
Alcohol reflux extracts, alcohol percolation extracts or decocting boils, wherein:
The alcohol reflux extracting method is:
Get the Chinese medicinal material of sarcandra glaber coarse powder, make solvent, flood after 1 hour with 6～10 times of amounts of 35%～95% ethanol, heating and refluxing extraction 2～4 times, each 1～4 hour, reclaim ethanol, drying promptly gets total extract;
The alcohol percolation extracting method is:
Get the Herba Sarcandrae coarse powder, make solvent with 25%～95% ethanol, behind the dipping, carry out percolation with 1～7ml/ minute speed, collect percolate, reclaim ethanol, drying promptly gets total extract;
Decocting the method for extracting is:
Get Chinese medicinal material of sarcandra glaber and add 6～10 times of water gagings decoctions, each 1～3 hour, filter, filtrate merges, and concentrates, and is drying to obtain total extract;
Separation and purification:
Total flavones and monomer whose effective ingredient can select following a kind of method extraction to obtain:
Macroreticular resin absorbing method, supercritical extraction or organic solvent extraction method, wherein:
The organic solvent extraction method:
Organic solvent ethyl acetate method is extracted the total flavones in the Herba Sarcandrae dry extract: water extracts the dried cream ultrasonic dissolution of Herba Sarcandrae repeatedly with ethyl acetate, gets total flavones;
Supercritical extraction:
The Herba Sarcandrae total extract is inserted in the supercritical extraction device, regulates flow, and pressure 20-50MPa, temperature 100-350 ℃, time 60-120min get the extract total flavones;
Macroreticular resin absorbing method:
Macroporous adsorbent resin extracts the total flavones in the Herba Sarcandrae dry extract: get the total extractum of Herba Sarcandrae, behind the dilute with water, the reuse constant flow pump pumps into pretreated macroporous adsorbent resin HBD-100 macroporous absorption, wash post with water, washing is back with 50～90% ethanol elutions, collect eluent, reclaim ethanol, dry that solid content is total flavones;
Drying means:
Flavone extract behind the separation and purification can adopt oven drying method, boulton process or spray drying method.
The extraction separation of total saponins:
The total saponins total extract can select following a kind of method extraction to obtain:
Alcohol reflux extracts, alcohol percolation extracts or water boiling and extraction, wherein:
The alcohol reflux extracting method is:
Get the Chinese medicinal material of sarcandra glaber coarse powder, doubly measure with 35%-95% ethanol 6-10 and make solvent, flood after 1 hour heating and refluxing extraction 2-4 time, each 1-4 hour, reclaim ethanol, concentrated solution reclaims organic solvent through organic solvent extraction, macroporous adsorbent resin is handled, and drying promptly gets total extract;
The alcohol percolation extracting method is:
Get the Herba Sarcandrae coarse powder, make solvent, behind the dipping, carry out percolation, collect percolate, reclaim ethanol with 1-7ml/ minute speed with 25%-95% ethanol; Concentrated solution reclaims organic solvent through organic solvent extraction, and macroporous adsorbent resin is handled, and drying promptly gets total extract;
Decocting the method for extracting is:
Get Chinese medicinal material of sarcandra glaber and add 6-10 times of water gaging and decoct, each 1-3 hour, filter, filtrate merges, and concentrates, and concentrated solution reclaims organic solvent through organic solvent extraction, and macroporous adsorbent resin is handled, and is drying to obtain total extract.
Separation and purification:
Total saponins and monomer whose effective ingredient can select following a kind of method extraction to obtain:
Macroreticular resin absorbing method, supercritical extraction or organic solvent extraction method, wherein:
Macroreticular resin absorbing method is:
Total extract is handled with ethyl acetate earlier, removes liposoluble substance; The total saponins of reuse n-butanol extraction water layer; N-butyl alcohol extract reclaims organic solvent, further removes impurity through the macroporous adsorbent resin enrichment; The macroporous adsorbent resin of enrichment total saponins 70% ethanol elution, 3-5 times of column volume of eluent consumption, ethanol is reclaimed in eluate, and drying gets total saponins.
Drying means:
Total saponin extracts behind the separation and purification of the present invention can adopt oven drying method, boulton process, spray drying method or freeze-drying.
The separation of polysaccharide effective site:
Chinese medicine Herba Sarcandrae polysaccharide extract method of the present invention:
Decoction and alcohol sedimentation technique: get Chinese medicinal material of sarcandra glaber, decocting filters, and uses ethanol precipitation, and is centrifugal, taking precipitate.Repeatedly several times, precipitate with ethanol filters again, drying, and dehydrated alcohol, acetone are washed, and drying gets the polysaccharide position.
Macroreticular resin absorbing method: get Chinese medicinal material of sarcandra glaber, decocting filters, and ethanol precipitation 24-48 hour, centrifugal, taking precipitate was dissolved in water, by macroporous resin, and washing.Eluate is immersed with ethanol, and repeatedly several times, precipitate with ethanol filters again, and dehydrated alcohol, acetone are washed, drying, get the polysaccharide position.
Macroporous resin adsorption, partition method: get the total extractum of Herba Sarcandrae, behind the dilute with water, by macroporous adsorptive resins, wash post with water, effluent is merged into solution A when washing post liquid with absorption.Washing back ethanol elution is collected eluent, isolating solution A is pumped into adsorption column adsorb.Absorption finishes, the washing post.Effluent when washing post liquid with absorption merges, and drying gets solid content and is the polysaccharide position.
The described application that contains the pharmaceutical composition of Herba Sarcandrae extract is characterized in that being applied to antitumor action, the efficacy enhancing and toxicity reducing effect, and antitumor is put, the toxic reaction of chemotherapy comprises and alleviates leukopenia and thrombocytopenia.
The described application that contains the pharmaceutical composition of Herba Sarcandrae extract is characterized in that being applied to treat bleeding due to blood-heat, ecchymosis, idiopathic thrombocytopenic purpura and secondary thrombocytopenic purpura, increased platelets counts.
The described application that contains the pharmaceutical composition of Herba Sarcandrae extract is characterized in that being applied to antimicrobial antiphlogistic, treatment pharyngolaryngitis, tracheobronchitis, pneumonia, keratitis, cellulitis, appendicitis.
The specific embodiment
Describe embodiment of the present invention below in detail.
One, the extraction separation of total flavone part and composition and assay
Chinese medicine Herba Sarcandrae flavone class total extract of the present invention can alcohol reflux extracts by Herba Sarcandrae is carried out, alcohol percolation extracts or water boiling and extraction obtains, wherein:
A, alcohol reflux extracting method are: get the Chinese medicinal material of sarcandra glaber coarse powder, doubly measure with 35%-95% ethanol 6-10 and make solvent, flood after 1 hour, and heating and refluxing extraction 2-4 time, each 1-4 hour, reclaim ethanol, drying promptly gets total extract;
B, alcohol percolation extracting method are: get the Herba Sarcandrae coarse powder, make solvent with 25%-95% ethanol, behind the dipping, carry out percolation with 1-7ml/ minute speed, collect percolate, reclaim ethanol, drying promptly gets total extract;
The method that C, decoction are extracted is: gets Chinese medicinal material of sarcandra glaber and adds 6-10 times of water gaging decoction, and each 1-3 hour, filter, the filtrate merging concentrates, and is drying to obtain total extract.
Separation and purification: above-mentioned A, B, C Herba Sarcandrae extract, any a kind obtains total flavones through organic solvent extraction method or absorption with macroporous adsorbent resin method or supercritical extraction separation and purification again.
The machine solvent extraction method: organic solvent ethyl acetate method is extracted the total flavones in the Herba Sarcandrae dry extract: with a certain amount of water with the dried cream ultrasonic dissolution of Herba Sarcandrae, extract repeatedly with a certain amount of ethyl acetate, ethyl acetate adopts 3 factors, the extraction of technology road is determined in the test of 3 horizontal quadratures, get content of total flavone greater than 50%, the response rate of total flavones is more than 80%.
Supercritical extraction: Herba Sarcandrae extract, insert in the supercritical extraction device, adjusting flow, pressure 20MPa, temperature 350C, time 120min get extract.Measure the general flavone content in the extract, the response rate of total flavones.The response rate total flavones amount of total flavones is greater than 50%, and the response rate of total flavones is more than 80%.
Macroreticular resin absorbing method: macroporous adsorbent resin extracts the total flavones in the Herba Sarcandrae dry extract: get the total extractum of Herba Sarcandrae, behind the dilute with water, the reuse constant flow pump pumps into pretreated macroporous adsorbent resin HBD-100 macroporous absorption.Wash post with water, washing back 50-90% ethanol elution is collected eluent, reclaims ethanol, and dry that solid content is total flavones, the content of flavone is greater than 50%, and the response rate of total flavones is more than 80%.
Determination of total flavonoids: the reference substance solution preparation: precision takes by weighing the control substance of Rutin 100mg of 105 ℃ of drying under reduced pressure to constant weight, put in the 100ml volumetric flask, add 60% ethanol 70ml, put slight fever dissolving in the water-bath, put cold, add 60% ethanol dilution to scale, shake up, the accurate 10ml that draws, put in the 50ml volumetric flask, add water to scale, shake up, promptly.
Standard curve preparation: the accurate reference substance solution 1.0,2.0,3.0 of drawing, 4.0,5.0, put respectively in the 25ml measuring bottle with 6.0ml, respectively add water 5ml, add 5% sodium nitrite solution 1ml, shake up, placed 6 minutes, add 10% sodium nitrate solution 1ml, shake up, placed 6 minutes, hydro-oxidation sodium test solution 10ml, add water to scale again, shake up, placed 15 minutes, do blank with method with 6ml water, measure trap according to spectrophotography at the wavelength place of 500nm, with the trap is vertical coordinate, and concentration is abscissa, the drawing standard curve.
The need testing solution preparation: precision takes by weighing total extract 20mg, puts in the 25ml volumetric flask, adds 70% ethanol 10ml, dissolving, and thin up is settled to scale, shakes up, promptly.The accurate 1ml that draws, put in the 25ml measuring bottle, method under the sighting target directrix curve preparation is operated from " respectively adding water 5ml ", with need testing solution 1ml in accordance with the law, thin up is done blank to 25ml, filter, get filtrate and measure trap in accordance with the law, read the weight of rutin the need testing solution from standard curve, calculate, promptly.
Total flavonoid calculates with rutin and contains the purity that reaches more than 50% to 99% after measured.
Drying means: the flavone extract behind the separation and purification of the present invention can adopt oven drying method, boulton process, spray drying method.Oven drying method, boulton process are long drying time, must be predrying in water-bath before the vacuum drying, with moisture Control in 20%, easy-to-drawly during vacuum drying driedly become cellular, drying can be finished in 2-3 days, otherwise, the water content height can overflow during vacuum drying, and the oven drying method required time is longer.The spray drying time is short, can finish in a few hours.How three kinds of methods are selected, visual physical condition.
Two, the extraction separation of total saponins
Chinese medicine Herba Sarcandrae total saponin extracts of the present invention can alcohol reflux extracts by Herba Sarcandrae is carried out, alcohol percolation extracts or water boiling and extraction obtains, wherein:
The alcohol reflux extracting method is: get the Chinese medicinal material of sarcandra glaber coarse powder, doubly measure with 35%-95% ethanol 6-10 and to make solvent, flood after 1 hour heating and refluxing extraction 2-4 time, each 1-4 hour, reclaim ethanol, concentrated solution reclaims organic solvent through organic solvent extraction, and macroporous adsorbent resin is handled, drying promptly gets total extract;
The alcohol percolation extracting method is: get the Herba Sarcandrae coarse powder, make solvent with 25%-95% ethanol, behind the dipping, carry out percolation with 1-7ml/ minute speed, collect percolate, reclaim ethanol; Concentrated solution reclaims organic solvent through organic solvent extraction, and macroporous adsorbent resin is handled, and drying promptly gets total extract;
The method of decoct extracting is: gets Chinese medicinal material of sarcandra glaber and adds 6-10 times of water gaging and decoct, and each 1-3 hour, filter, filtrate merges, and concentrates, and concentrated solution reclaims organic solvent through organic solvent extraction, and macroporous adsorbent resin is handled, and is drying to obtain total extract.
Separation and purification: the extract that obtains in the preparation method of the present invention can be removed impurity with imitating ground through separation and purification, with the enrichment effectively of total saponins position, improves the activity and the drug effect of total extract significantly.Separation and refining method of the present invention is a macroreticular resin absorbing method.Also available supercritical extraction and organic solvent extraction obtain total saponins and monomer whose effective ingredient.
Total extract is handled with ethyl acetate earlier, removes liposoluble substance; The total saponins of reuse n-butanol extraction water layer; N-butyl alcohol extract reclaims organic solvent, further removes impurity through the macroporous adsorbent resin enrichment; The macroporous adsorbent resin of enrichment total saponins 70% ethanol elution, 3-5 times of column volume of eluent consumption, ethanol is reclaimed in eluate, and drying gets total saponins and monomer whose effective ingredient.
Total saponin content is measured: total saponins is contrast with Rb1, determined by ultraviolet spectrophotometry, and total saponin content is greater than 50% to 98%.The configuration of reference substance test solution: precision takes by weighing ginsenoside Rb
1Reference substance 5mg puts in the 5ml measuring bottle, adds methanol and puts scale, shakes up, and makes the reference substance solution of ginsenoside Rb1 1mg/ml.
Determining of standard curve: the accurate ginsenoside of absorption Rb
1Reference substance (1mg/ml) 30,60,90,120,150ul put in the tool plug test tube, and the same step of operational approach is measured each absorbing wavelength curve plotting result, ginsenoside Rb in the 550nm place
1Reference substance concentration is (linear between 8～45ug/ml).The calculating regression equation is Y=0.01825X-0.0024r=0.9987.The assay of sample: precision takes by weighing with-batch sample and measures trap by the method in " mensuration of standard curve ", and according to the content of ginsenoside in the regression equation calculation total saponins.
Total saponins calculates with the ginsenoside and contains the purity that reaches more than 50% to 99% after measured.
Drying means: the total saponin extracts behind the separation and purification of the present invention can adopt oven drying method, boulton process, spray drying method, lyophilization.Oven drying method, boulton process are long drying time, must be predrying in water-bath before the vacuum drying, with moisture Control in 20%, easy-to-drawly during vacuum drying driedly become cellular, drying can be finished in 2-3 days, otherwise, the water content height can overflow during vacuum drying, and the oven drying method required time is longer.The spray drying time is short, can finish in a few hours.Lyophilization elder generation concentrating under reduced pressure, lyophilization again, this method helps to preserve the activity of determination system of thermal unstable material.How four kinds of methods are selected, visual physical condition.
Three, the separation of polysaccharide effective site and assay
The separation of polysaccharide effective site: Chinese medicine Herba Sarcandrae polysaccharide extract method of the present invention can obtain by Herba Sarcandrae is carried out alcohol reflux extraction, alcohol percolation or water boiling and extraction with aforementioned.
1, decoction and alcohol sedimentation technique: get Chinese medicinal material of sarcandra glaber, decocting 1-3 hour, filter, be concentrated to certain density, use 60-80% ethanol precipitation 24-48 hour, centrifugal, taking precipitate.Repeatedly several times, add activated carbon treatment, precipitate with ethanol filters again, drying, and dehydrated alcohol, acetone are washed, and drying gets white powder, is the polysaccharide position.
2, macroreticular resin absorbing method: get Chinese medicinal material of sarcandra glaber, decocting 1-3 hour, filter, be concentrated to certain density, use 60-80% ethanol precipitation 24-48 hour, centrifugal, taking precipitate is dissolved in water, by macroporous resin (AB-8 type or other of this type), washing.Eluate is immersed with ethanol, repeatedly several times, adds activated carbon treatment, and precipitate with ethanol filters again, and dehydrated alcohol, acetone are washed, drying, get white powder, are the polysaccharide position.
3, macroporous resin adsorption, partition method: get the total extractum of Herba Sarcandrae, behind the dilute with water, adsorb by macroporous adsorptive resins.Wash post with water, effluent is merged into solution A when washing post liquid with absorption.Eluent is collected with 3 times of column volume 70% ethanol elutions in the washing back, reclaims ethanol, and the dry solid content that gets pumps into the macroporous resin adsorption post with isolating solution A and adsorbs.Absorption finishes, with the washing post of 3 times of column volumes.Effluent when washing post liquid with absorption merges, and drying gets solid content and is the polysaccharide position.
Determination of polysaccharide: the preparation of glucose standard stock solution: precision takes by weighing the glucose 100mg that is dried to constant weight, and 10 its concentration of water dissolution and standardize solution are 1.0mg/ml, and its concentration dilution is reference substance solution for 100 times.The preparation of phenol liquid: take by weighing phenol 100g in flask, add the 0.1g aluminium flake, the 0.05g sodium carbonate adds thermal distillation, collects 182 ℃ of fraction 10g, and adding distil water 190g dissolving places brown bottle standby.The standard curve preparation: accurate absorption standard stock solution 5mL water standardize solution is 25mL, gets 1.0,2.0,3.0,4.0 respectively, and the 5.0ml standardize solution is 25ml.Get 1.0ml more respectively and in tool plug test tube, respectively add phenol liquid 1.0ml, drip concentrated sulphuric acid 5.0ml rapidly, in addition with the same operation of 1.0ml water, as blank.Room temperature is placed 30min, surveys its absorbance in its maximum absorption wavelength λ max=490nm place.The preparation of sample liquid: accurately measure 5ml Herba Sarcandrae extractum, add in the flask that the 95ml dehydrated alcohol is housed, heating in water bath is to clarification, abandoning supernatant, volatilize ethanol, precipitation is with the water dissolution of 30ml (if having on the wall, then ultrasonic make it is molten), and solution is with Sevage method removal albumen, supernatant is made into 80% solution with dehydrated alcohol, placement is spent the night, filter (trickle because of precipitating, easily gone over by sucking filtration, filter with funnel), precipitation is used dehydrated alcohol respectively, acetone, ether washing, after flinging to organic solvent, to precipitate together with filter paper one and reinstate distilled water wash, and ultrasonicly make the precipitation on the paper fully dissolve, filter, it is colourless being washed till filtrate, filtrate is transferred in the 250ml measuring bottle in the lump, and standardize solution is standby.Measurement of the polysaccharide content: the accurate sample liquid 2.0ml that draws is in the 50ml measuring bottle, and standardize solution is drawn 1.0mL again and operated by the step in 7.3, measures its absorption value, and the content of sample polysaccharide calculates (calculating with glucose) according to following formula.Polyoses content (mg/ml)=A sample/A is right * concentration * extension rate of glucose reference substance.
Record after measured and to calculate polysaccharide with glucose and contain the purity that reaches more than 50% to 99%.
Four, the separation of monomeric compound
The present invention separates from the total flavone part that separation makes and obtains 4 chemical compound (I
A, I
B, I
C) and carried out preliminary structure and identified, wherein 3 are new discovery, 1 is known.
Compound I
A: white crystal, mp212.2 ℃.UV(MeOH)λmax 338nm、295nm、230nm、215nm。IR (KBr): 1716 (COO-), 1600-1500 (phenyl ring).
1Proton signal δ 7.96 among the H-NMR (1H, d is J=9.6Hz) with 6.40 (1H, d, J=9.6Hz) show on the phenyl ring two protons of adjacent idol, (3H s) shows the existence of two methoxyl groups to δ 3.92 and 3.82,7.13 (1H s) is proton on the phenyl ring, and δ 3.0-4.0 shows that sugar goes up proton.
13δ 159.7,149.3 among the C-NMR, and 144.3,142.3,141.6,140.2,114.6 114.4 and 105.52 have shown the coumarin parent nucleus, δ 102.1,77.4,76.4,74.1,69.9 and 60.8 be the signal of carbon on one group of sugar, therefore this chemical compound is the monoglycosides of coumarin, because the coupling constant of the terminal hydrogen δ 5.17 of sugar is 6.8Hz, infers that it is the β glucose that institute connects sugared.So this chemical compound of Preliminary Identification is isofraxidin-7-O-glucoside.
Compound I
A. structure
Compound I
B: khaki crystal, mp136.9 ℃.UV(MeOH)λmax331nm、 293nm、212nm。IR (KBr): 1600-1500 (phenyl ring).
1H-NMR (DMSO) δ: 7.05 ~ 6.5 is hydrogen on the phenyl ring, 4.99 (1H, dd, J=4,9Hz, H-2), 3.07 (1H, dd, H-3trans), 2.86 (1H, dd, H-3cis).
13C-NMR(DMSO)δ：74.1(C-2)，36.9(C-3)，171.8(C-4)，166.4(C-5)，114.2(C-6)，149.0(C-7)，115.4(C-8)，146.1(C-9)，115.8(C-10)，145.8(C-1’)，145.4(C-2’，6’)，145.3(C-3’，5’)，128.5(C-4’)。Identify that this chemical compound is 5,7-dihydroxy flavanone according to spectrum and relevant information.
Compound I
B. structure
Compound I
C: glassy yellow crystal, mp77.2 ℃.UV(MeOH)λmax333nm、210nm。IR (KBr): 1600-1500 (phenyl ring).
1H-NMR (DMSO) δ: 7.46 (1H, d, J=15.6Hz, H-β α), 6.25 (1H, d, J=15.6Hz, H-α), 7.50 ~ 6.48 is hydrogen on the phenyl ring, 3.61 (3H, s, OCH
3).
13C-NMR(DMSO)δ：72.7(C-α)，51.9(C-β)，169.9(C＝O)，106.7(C-1’)，146.3(C-2’)，96.8(C-3’)，165.8(C-4’)，91.8(C-5’)，148.7(C-6’)，145.5(C-1)，144.9(C-2，6)，126.6(C-3，5)，144.0(C-4)，36.2(OCH
3)。Identify that according to spectrum and relevant information this chemical compound is 2 ', 6 '-dihydroxy-4 '-methoxyl group chalcone derivative.
Compound I
C. structure
In addition, also be separated to known compound astilbin (astibin).
Five, white platelet-increasing role is used and risen to the antitumor of total flavone valid target, effective ingredient and total saponins effective site, effective ingredient, polysaccharide effective site and antineoplastic efficacy enhancing and toxicity reducing
(1) integral experiment: by to the kinds of tumors evidence, flavone effective part, effective ingredient and effective part of saponin, the polysaccharide effective site that we propose and be mixed with injection, tablet etc. direct antineoplastic action is arranged.
1, direct anti-tumor experiment: at direct anti-mice S
180In the solid tumor test and at direct anti-mice S
180In the test of ascitic type tumor, by oral, lumbar injection, intramuscular injection, these four kinds of modes of tail vein injection are given Herba Sarcandrae flavone effective site, effective ingredient (isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether) and effective part of saponin, experimental result shows that positive control Western medicine cyclophosphamide has obvious antineoplastic, flavone effective part, effective ingredient and effective part of saponin, the tumour inhibiting rate of polysaccharide effective site makes S between 30% and 80%
180The increase in life span 30-90% of ascitic type mice with tumor., antineoplastic action is arranged.
Table 1 Herba Sarcandrae flavone effective site antitumor S
180The result (x ± s, n=10)
| Group | Route of administration | Dosage (mg/kg) | Tumor heavy (g) | Suppression ratio (%) |
| Normal saline | iv | 0.1ml/10g | 1.7898 | |
| Cyclophosphamide | ip | 80mg/kg | 0.08301 | 95％ |
| Herba Sarcandrae flavone | iv | 100mg/kg | 1.2216 | 32％ |
2, synergism experiment: cyclophosphamide treatment mice S
180In the solid tumor synergism test, mice S
180In the ascitic type tumor synergism test, by oral, lumbar injection, intramuscular injection, it is that 20mg/kg adds respectively and uses Herba Sarcandrae flavone effective site that these four kinds of mode administration cyclophosphamide of tail vein injection reduce dosage 20mg/kg and cyclophosphamide dosage, effective ingredient (isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether) and effective part of saponin, polysaccharide effective site, experimental result shows single tumour inhibiting rate of using cyclophosphamide between 5% and 20%, and increase in life span is between 16% and 50%.Herba Sarcandrae flavone effective site, effective ingredient and effective part of saponin, polysaccharide effective site tumour inhibiting rate illustrate when Herba Sarcandrae flavone effective site, effective ingredient, polysaccharide effective site and effective part of saponin and cyclophosphamide share obviously to strengthen chemotherapeutic cyclophosphamide antitumor action between 30% and 70%.
Table 2 Herba Sarcandrae flavone effective site antitumor S
180The synergism experiment result (x ± s, n=10)
| Group | Route of administration | Dosage (mg/kg) | Tumor heavy (g) | Suppression ratio (%) |
| Normal saline | iv | 0.1ml/10g | 1.9810 | |
| Cyclophosphamide | ip | 20mg/kg | 1.6381 | 17％ |
| Cyclophosphamide 20mg/kg+ flavone | ip+iv | 100mg/kg | 1.1022 | 44％ |
3, attenuation experiment: at the flavone of (50% to 99%) purity more than 50% to cyclophosphamide, in the test of cytosine arabinoside treatment mice S180 solid tumor attenuation, by oral, lumbar injection, intramuscular injection, these four kinds of mode administration cyclophosphamide of tail vein injection, cytosine arabinoside and add Herba Sarcandrae flavone effective site respectively, effective ingredient (isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether) and effective part of saponin, polysaccharide effective site.Experimental result shows that mice all platelet occurs behind administration cyclophosphamide, cytosine arabinoside and leukocyte significantly descends, after adding Herba Sarcandrae flavone effective site, effective ingredient and effective part of saponin, polysaccharide effective site respectively, leukocyte and platelet significantly rise, and illustrate that Herba Sarcandrae flavone effective site, effective ingredient and effective part of saponin, polysaccharide effective site and chemotherapeutic have tangible Attenuation when share.
(2) experiment in vitro
1, to cultured tumor cells in vitro growth inhibited effect experiment 1: at mice S to In vitro culture
180In the painted experiment of growth inhibited effect of sarcoma cell, Herba Sarcandrae flavone effective site, effective ingredient and effective part of saponin, experimental result shows Herba Sarcandrae flavone effective site, effective ingredient and effective part of saponin: isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether to the suppression ratio of above-mentioned growth of tumour cell between 20% to 95%, flavone effective part is described, effective ingredient and effective part of saponin: isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether has antitumor action.
Table 3 Herba Sarcandrae is external to mice S
180The suppression ratio of tumor cell (RPMI-1640 culture fluid trypan blue liquid dyeing counting indigo plant is dyed rate)
| Group | Concentration (μ g/ml) | 24h suppression ratio (%) |
| RPMI-1640 flavone effective part polysaccharide active component effective part of saponin isofraxidin-7-O-glucoside 5; 7-dihydroxy flavanone 2 '; 6 '-dihydroxy-4 '-the different U.S. five-leaved pine flavanone dihydromyricetin hoof line pelargonin glycosides astilbin naringenin 4 of methoxyl group chalcone ', the 7-dimethyl ether | 0 10 10 10 5 5 5 5 5 5 5 5 | 0 36 35 33 32 32 31 35 35 33 35 30 |
2, external bacteriostatic experiment: in extracorporeal bacteria inhibitor test, adopt bacillus pyocyaneus, pneumobacillus, Bacillus proteus, escherichia coli, Candida albicans, staphylococcus aureus, dysentery bacterium, Bacillus typhi, paratyphoid bacillus A, the first streptococcus, micrococcus catarrhalis, hemophilus influenza, Diplococcus pneumoniae, 15 kind of 117 strain bacterium such as streptococcus and bacteroides fragilis, show flavone effective part through MIC and MSC test, effective ingredient (isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether) and effective part of saponin in various degree antibacterial action is arranged.
Claims (5)
1, a kind of pharmaceutical composition that contains Herba Sarcandrae extract, it is characterized in that it contains effective site and/or the effective ingredient that extracts from Herba Sarcandrae, comprise flavone, and/or saponin, and/or the effective site of polysaccharide, or in the effective ingredient of following flavone one or several: isofraxidin-7-O-glucoside, 5,7-dihydroxy flavanone, 2 ', 6 '-dihydroxy-4 '-the methoxyl group chalcone derivative, different U.S. five-leaved pine flavanone, dihydromyricetin, hoof stricture of vagina pelargonin glycosides, astilbin, naringenin 4 ', the 7-dimethyl ether, the purity of the effective site that extracts in the described Herba Sarcandrae is 50% to 99%, and the purity of the effective ingredient that extracts in the described Herba Sarcandrae is 85% to 99%.
2, the pharmaceutical composition that contains Herba Sarcandrae extract according to claim 1 is characterized in that the form of described compositions comprises: tablet: comprise general oral, buccal tablet, chewable tablet, injection: comprise small-volume injection, big injection, injectable powder, Emulsion, suspension, pill, drop pill, capsule and soft capsule, granule, effervescent, oral liquid, syrup, Emulsion, mixture, slow releasing agent, controlled release agent, targeting preparation and other various preparations.
3, the application that contains the pharmaceutical composition of Herba Sarcandrae extract according to claim 1 and 2 is characterized in that being applied to antitumor action, the efficacy enhancing and toxicity reducing effect, and antitumor is put, the toxic reaction of chemotherapy comprises and alleviates leukopenia and thrombocytopenia.
4, the application that contains the pharmaceutical composition of Herba Sarcandrae extract according to claim 1 and 2 is characterized in that being applied to treat bleeding due to blood-heat, ecchymosis, idiopathic thrombocytopenic purpura and secondary thrombocytopenic purpura, increased platelets counts.
5, the application that contains the pharmaceutical composition of Herba Sarcandrae extract according to claim 1 and 2 is characterized in that being applied to antimicrobial antiphlogistic, treatment pharyngolaryngitis, tracheobronchitis, pneumonia, keratitis, cellulitis, appendicitis.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101665479B (en) * | 2009-09-22 | 2012-05-16 | 三明华健生物工程有限公司 | Process for synchronously extracting isofraxidin and flavonoid compounds from sarcandra glabra and application thereof |
| CN102603907A (en) * | 2012-01-17 | 2012-07-25 | 中国药科大学 | Glabrous sarcandra herb polysaccharide and preparation method and application thereof |
-
2006
- 2006-01-18 CN CN 200610049219 patent/CN1839903A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101665479B (en) * | 2009-09-22 | 2012-05-16 | 三明华健生物工程有限公司 | Process for synchronously extracting isofraxidin and flavonoid compounds from sarcandra glabra and application thereof |
| CN102603907A (en) * | 2012-01-17 | 2012-07-25 | 中国药科大学 | Glabrous sarcandra herb polysaccharide and preparation method and application thereof |
| CN102603907B (en) * | 2012-01-17 | 2014-04-02 | 中国药科大学 | Glabrous sarcandra herb polysaccharide and preparation method and application thereof |
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